- Synthesis of Modified RGD-Based Peptides and Their in vitro Activity
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Arg-Gly-Asp (RGD) peptides represent the most outstanding recognition motif involved in cell adhesion that binds to the αvβ3 integrin, which has been targeted for cancer therapy. Various RGD-containing peptides and peptidomimetics have been designed and synthesized to selectively inhibit this integrin. In this study, the synthesis of RGD-based peptides through the incorporation of the short bioactive peptide Phe-Ala-Lys-Leu-Phe (FAKLF) at the C and N termini of RGD has been achieved by using a solid-phase peptide synthesis approach. The peptides were purified by means of preparative RP-HPLC and their structures were confirmed through HRMS (ESI). The MTT assay revealed that the RGD and FAKLF peptides inhibited the proliferation of human umbilical vein endothelial cells (HUVECs) in a dose-dependent manner, with IC50 values of 3000 and 500 ng mL?1, respectively. Interestingly, a drastic improvement was observed in the antiproliferative activity of the combined structures of the FAKLFRGD and RGDFAKLF peptides, leading to IC50 values of 200 and 136.7 ng mL?1, respectively. Meanwhile, based on apoptosis results, the potential of peptides to induce apoptosis, in accordance with their antiproliferative activity, indicated that the RGD and FAKLF peptides, and the peptides synthesized based on their combinations induced cell apoptosis in a dose-dependent manner followed by inhibition of the proliferation of endothelial cells. Moreover, the incorporation of d-leucine increased the induction of apoptosis by these peptides.
- Hamdan, Fatima,Bigdeli, Zahra,Asghari, S. Mohsen,Sadremomtaz, Afsaneh,Balalaie, Saeed
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supporting information
p. 282 - 288
(2019/01/14)
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- Arg-Gly-Asp (RGD) Sequence Containing Cyclic Peptide and Its Active Targeting Liposomes
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The present invention relates to the field of pharmaceutics and clinical pharmacy, involving the preparation method and application of a cyclic peptide containing Argnine-Glycine-Aspartate sequence and its active targeting liposomes. The cyclic peptide described here meets the requirement for ligand in that it forms ring by amide linkage with stable sterical structure, it shows low propensity to degrade, and it carries an active hydrosulfide group which is easy to modify carriers. The artificially synthesized peptide, which has a small molecular weight and low propensity to cause immune response, can be used as the ligand to bind with the integrin on the surface of HSC. The active targeting liposome established with the cyclic peptide realized cell-targeted therapy of experimental hepatic fibrosis via receptor-mediated pathway. The invention can target RGD cyclic peptide-labeled interferon-loaded liposomes to the fibrotic liver and its good efficacy in the treatment of hepatic fibrosis has been proven by experiments in rats in vitro and in vivo.
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- Preparation and biological activities of a bivalent poly(ethylene glycol) hybrid containing an active site and its synergistic site of fibronectin.
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A bivalent poly(ethylene glycol) or PEG hybrid of fibronectin-related peptides was prepared. An active site peptide (RGD) and its synergistic site peptide (PHSRN) of fibronectin were conjugated with an amino acid-type PEG (aaPEG) to form PHSRN-aaPEG-RGD.
- Susuki, Yuichi,Hojo, Keiko,Okazaki, Ikuko,Kamata, Haruhiko,Sasaki, Masahiko,Maeda, Mitsuko,Nomizu, Motoyoshi,Yamamoto, Yoko,Nakagawa, Shinsaku,Mayumi, Tadanori,Kawasaki, Koichi
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p. 1229 - 1232
(2007/10/03)
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- Tripeptides useful as immunostimulants as well as in the prevention of metastases
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The present invention is referred to tripeptides having the following general formula: where X=L-Arg or D-Arg and Y=L-Asp or D-Asp. These tripeptides, endowed with both immunostimulant and antimetastatic properties, are active not only after parenteral administration, but also after oral treatment. The invention is also related to the procedure for the preparation of said compounds.
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